The direct release of nitric oxide by gypenosides derived from the herb Gynostemma pentaphyllum

Nitric Oxide. 1999 Oct;3(5):359-65. doi: 10.1006/niox.1999.0245.


Herbal medicines are increasingly being utilized to treat a wide variety of disease processes. Gypenosides are triterpenoid saponins contained in an extract from Gynostemma pentaphyllum and are reported to be effective in the treatment of cardiovascular diseases; however, the mechanism underlying the therapeutic effect is not known. We tested the hypothesis that gypenosides extracted from G. pentaphyllum elicit vasorelaxation through the direct release of endothelium-derived nitric oxide. Nitric oxide production in bovine aortic endothelial cells grown under standard tissue culture conditions was quantitated using a chemiluminescence method. Arterial vasomotion was assayed using isolated porcine coronary artery rings under standard isometric recording conditions. The extract of G. pentaphyllum at 0.1-100 microg/ml elicited concentration-dependent vasorelaxation of porcine coronary rings that was antagonized by the nitric oxide synthase inhibitor N(G)-nitro-l-arginine methyl ester. Indomethacin had no significant effect on G. pentaphyllum-induced relaxation. The G. pentaphyllum extract elicited a concentration-dependent increase in nitric oxide production from cultured bovine aortic endothelial cells. At the concentrations utilized, there was no morphological evidence for cellular toxicity. These results demonstrate that extracts of G. pentaphyllum directly stimulate nitric oxide release, but not prostanoid production. Nitric oxide production in response to gypenosides may be one mechanism whereby this herbal medicine elicits its therapeutic effects.

MeSH terms

  • Animals
  • Aorta / drug effects
  • Cattle
  • Cells, Cultured
  • Coronary Vessels / drug effects
  • Drugs, Chinese Herbal / metabolism*
  • Endothelium, Vascular / cytology
  • Endothelium, Vascular / drug effects
  • Enzyme Inhibitors / pharmacology
  • In Vitro Techniques
  • NG-Nitroarginine Methyl Ester / pharmacology
  • Nitric Oxide / metabolism*
  • Nitric Oxide Synthase / antagonists & inhibitors
  • Plant Extracts / metabolism*
  • Saponins / metabolism*
  • Swine
  • Terpenes / metabolism*
  • Vasodilation / drug effects*


  • Drugs, Chinese Herbal
  • Enzyme Inhibitors
  • Plant Extracts
  • Saponins
  • Terpenes
  • Nitric Oxide
  • Nitric Oxide Synthase
  • NG-Nitroarginine Methyl Ester